A7-Nicotinic receptor

Accumbens of the Rat Putative Role of a7 Nicotinic Receptors in the Ventral Tegmental Area." Neuroscience 85 1005-9. 

In general, diverse TA are known to bind to (a) muscarinic receptors (MR), (b) 5-hydroxytryptamine (serotonin) receptor 3 (5-HT3R), (c) al-adrenoreceptors (al-AR), or (d) a7-nicotinic receptors (a7-nAChR) thus causing different physiological effects. The corresponding mechanisms of action should briefly be addressed below. 

Blum LC, van Deursen R, Bertrand S et al (2011) Discovery of a7-nicotinic receptor ligands by virtual screening of the chemical universe database GDB-13. J Chem Inf Model 51(12) 3105-3112... 

The efficacy of a7-nicotinic receptor agonists has been assessed in multiple animal paradigms of learning and memory. For example, DMXB-A improves monkey performance on a delayed matching to sample task, an effect that persists for 24 h after drug administration (Briggs et al., 1996). DMXB-A... 

Fig. 10 Model of glutamate receptor Internalization through Ap-mediated activation of STEP. Ap activates the a7 nicotinic receptor, leading to Ca + influx and activation of calcineurin [197], Calcineurin subsequently dephosphorylates and activates STEP. Concomitantly, Ap also elevates STEP protein levels through inhibition of the ubiquitin proteasome system [203]. STEP dephosphorylates a regulatory tyrosine residue in both the NR2B and GluR2 glutamate receptor subunits, leading to internalization of the receptors [199,200]. As a result, synaptic function is disrupted (Figure from ref. 131, with permission)...

Wu H-Q, Pereira EFR, Bruno JP, Pellicciari R, Albuquerque EX, Schwarcz R (2010) The astrocyte-derived a7 nicotinic receptor antagonist kynurenic acid controls extracellular glutamate levels in the prefrontal cortex. J Mol Neurosci 40 204-210... 

Catecholaminergic terminals bear non-a7 nicotinic receptors, which are thought to be of either the j82 or the J34 type in the case of dopaminergic and noradrenergic terminals, respectively. A thorough review of the pharmacology of these receptors can be found in Kaiser and Wonnacott (229). 

Sekhon HS, Jia Y, Raab R, Kuryatov A, Pankow JF, Whitsett JA, et al. Prenatal nicotine increases pulmonary a7 nicotine receptor expression and alters fetal lung development in monkeys. J Clin Invest 1999 103 637-647. 

Scheme 4.39 Aldol addition of triphenyl glycol ester 173 to bicydic ketone 180 as the key step in a synthesis of the selective a7 nicotinic receptor agonist AR-R17779.

Kem, W.R. (2000) The brain a7 nicotinic receptor maybe an important therapeutic target for the treatment of Alzheimer s disease studies with DMXBA (GTS-21). Behav. Brain Res, 113,169-181. 

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